Crystal structure of the Rho-associated coiled-coil kinase 2 inhibitor belumosudil bound to CK2α.

ABSTRACT: The small molecule belumosudil was initially identified as a selective inhibitor of Rho-associated coiled-coil kinase 2 (ROCK2) and has recently been approved for the treatment of graft-versus-host disease. However, recent studies have shown that many of the phenotypes displayed upon treatment with belumosudil were due to CK2α inhibition. CK2α is in itself a very promising therapeutic target for a range of conditions and has recently been put forward as a potential treatment for COVID-19. Belumosudil presents a promising starting point for the development of future CK2α inhibitors as it provides a safe, potent and orally bioavailable scaffold. Therefore, several of the major hurdles in drug development have already been overcome. Here, the crystal structure of belumosudil bound to the ATP

SUBMITTER: Brear P 

PROVIDER: S-EPMC9527651 | biostudies-literature | 2022 Oct

REPOSITORIES: biostudies-literature